GNF179 Metabolite |
| カタログ番号GC36173 |
GNF179 代謝産物は、最適化された 8,8-ジメチル IP 類似体である GNF179 の代謝産物であり、in vitro 代謝安定性と in vivo 経口バイオアベイラビリティー (多剤耐性株 W2 に対して 4.8 nM) を示しました。
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Cas No.: 1310455-86-7
Sample solution is provided at 25 µL, 10mM.
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GNF179 metabolite is the metabolite of GNF179, which is an optimized 8,8-dimethyl IP analog that exhibited the potency(4.8 nM against the multidrug resistant strain W2) in vitro metabolic stability and in vivo oral bioavailability.IC50 value: Target: Anti-parasitic agentGNF179 exhibits a low clearance (CL=22 ml/min/kg, ~25% of hepatic blood flow in mice), a large volume of distribution (steady-state volume of distribution, Vss=11.8 l/kg), a moderate residence time (MRT=9 hours) and suitable terminal half-life (t1/2=8.9 hours). GNF179 reduced Plasmodium berghei parasitemia levels by 99.7% with a single 100 mg/kg oral dose, and prolonged mouse survival by an average of 19 days. GNF179 was able to protect against an infectious P. berghei sporozoite challenge with a single oral dose at 15 mg/kg while NITD609 was not.
[1]. Meister S, et al. Imaging of Plasmodium liver stages to drive next-generation antimalarial drug discovery. Science. 2011 Dec 9;334(6061):1372-7.
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